Title compds. I [R1 and R2 independently = H, CH3, or CH2CH3; R3 = H, CN, F, Cl, Ch3, OCH3, or CF3; each R4 independently = F, Cl, Br, CH3, OCH3, CF3, or CN; X = CH2 or CH2CH2; n = 0 to 2], and their pharmaceutically acceptable salts, are prepared and disclosed as aldosterone synthase inhibitors. Thus, e.g., II was prepared by cyclization of 4-(3,3-dimethyl-4-oxocyclopentyl)benzonitrile with N,N-dimethylformamide di-Me acetal. Select I were evaluated in aldosterone synthase (hcyp11B2) inhibition assays, e.g., II demonstrated an IC50 value of 0.005 µM.
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Note: Titles and abstracts for patent records in CAplus are routinely enhanced to better describe the claimed invention. In this example, CAS enhanced both the abstract and title using additional information found in the patent. The original title of the PCT patent publication is Pyrazole derivatives useful as aldosterone synthase inhibitors. For the CAplus record, this title was enhanced to read Preparation of pyrazole derivatives for use as aldosterone synthase inhibitors.